chlorcyclizine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
diphenylmethyl piperazine derivatives 593 82-93-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • chlorcyclizine
  • chlorcycline
  • chlorocycline
  • perazyl
  • chlorcyclizine hydrochloride
  • chlorcyclizine HCl
  • Molecular weight: 300.83
  • Formula: C18H21ClN2
  • CLOGP: 4.51
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 6.48
  • ALOGS: -3.85
  • ROTB: 3

Drug dosage:

DoseUnitRoute
0.10 g O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 3.585 High 0.88
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.443 High 0.88
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 18.408 10^-6 cm/s High 0.88
dh-clint Dog hepatocyte intrinsic clearance 18.030 uL/min/10^6 cells High 0.88
dppb Dog plasma protein binding (% unbound) 2.380 % High 0.88
fcs-ppb Fetal calf serum protein binding (% unbound) 7.310 % High 0.88
herg hERG pIC50 5.968 pIC50 High 0.88
hh-clint Human hepatocyte intrinsic clearance 5.035 uL/min/10^6 cells High 0.88
hlm-clint Human liver microsomal intrinsic clearance 14.997 uL/min/mg protein High 0.88
hppb Human plasma protein binding (% unbound) 2.510 % High 0.88
kinase-safety-class ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK 38
kinase-selectivity-class AKT3,AXL,PDK4,PRKG1,SIK2 5
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.156 High 0.88
mh-clint Mouse hepatocyte intrinsic clearance 46.026 High 0.88
mppb Mouse plasma protein binding (% unbound) 2.790 High 0.88
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.512 High 0.88
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 7.110 % High 0.88
rh-clint Rat hepatocyte intrinsic clearance 96.383 uL/min/10^6 cells High 0.88
rh-fuinc Rat hepatocyte fraction unbound in incubation 11.670 % High 0.88
rppb Rat plasma protein binding (% unbound) 3.280 % High 0.88
solubility-dd Solubility at pH 7.4 in DMSO 420.727 uM High 0.88

Approvals:

DateAgencyCompanyOrphan
None FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R06AE04 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Piperazine derivatives
CHEBI has role CHEBI:22587 antiviral agent

Related Drugs by ATC class:

R06AE Piperazine derivatives 6 drugs
buclizinecetirizinecyclizinelevocetirizinemeclozineoxatomide

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Vasomotor rhinitis indication 8229003 DOID:4730
Cough indication 49727002
Allergic rhinitis indication 61582004
Nasal discharge indication 64531003
Nasal congestion indication 68235000
Sneezing indication 76067001
Common cold indication 82272006 DOID:10459
Seasonal allergic rhinitis indication 367498001
Allergic conjunctivitis indication 473460002 DOID:11204
Ocular hypertension contraindication 4210003 DOID:9282
Dependent drug abuse contraindication 6525002
Peptic ulcer contraindication 13200003 DOID:750
Chronic disease of respiratory system contraindication 17097001
Mood swings contraindication 18963009
Myocardial infarction contraindication 22298006 DOID:5844
Inflammatory bowel disease contraindication 24526004 DOID:0050589
Ventricular tachycardia contraindication 25569003
Hyperthyroidism contraindication 34486009 DOID:7998
Acute hepatitis contraindication 37871000
Hypertensive disorder contraindication 38341003 DOID:10763
Disorder of gallbladder contraindication 39621005 DOID:0060262
Hypothyroidism contraindication 40930008 DOID:1459
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Chronic heart failure contraindication 48447003
Bradycardia contraindication 48867003
Acidosis contraindication 51387008
Coronary arteriosclerosis contraindication 53741008 DOID:3393
Arterial thrombosis contraindication 65198009
Drug AND/OR toxin-induced diarrhea contraindication 65979008
Substance abuse contraindication 66214007
Benign intracranial hypertension contraindication 68267002 DOID:11459
Arteriosclerotic vascular disease contraindication 72092001
Diabetes mellitus contraindication 73211009 DOID:9351
Urethral stricture contraindication 76618002
Decreased respiratory function contraindication 80954004
Injury of head contraindication 82271004
Chronic idiopathic constipation contraindication 82934008
Epilepsy contraindication 84757009 DOID:1826
Kidney disease contraindication 90708001 DOID:557
Acute abdominal pain contraindication 116290004
Procedure on urinary system contraindication 118677009
Partial atrioventricular block contraindication 195039008
Acute pancreatitis contraindication 197456007 DOID:2913
Disease of liver contraindication 235856003 DOID:409
Bladder outflow obstruction contraindication 236645006
Telangiectasia disorder contraindication 247479008
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Lesion of brain contraindication 301766008
Primary adrenocortical insufficiency contraindication 373662000
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Operation on gastrointestinal tract contraindication 386621005
Hypoxia contraindication 389086002
Angle-closure glaucoma contraindication 392291006 DOID:13550
Pseudomembranous enterocolitis contraindication 397683000
Atrophoderma contraindication 399979006
Peripheral vascular disease contraindication 400047006
Disorder of coronary artery contraindication 414024009
Central nervous system depression contraindication 418072004
Ultrarapid metabolizer due to cytochrome p450 CYP2D6 variant contraindication 422681000
Dysfunction of sphincter of Oddi contraindication 430887001
Hypertensive urgency contraindication 443482000
Acute exacerbation of asthma contraindication 708038006




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.19 Basic
pKa2 3.56 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Apoptosis regulator Bcl-2 Cytosolic other Kd 4.22 CHEMBL

External reference:

IDSource
4019672 VUID
N0000178900 NUI
14362-31-3 SECONDARY_CAS_RN
2354 RXNORM
C0008183 UMLSCUI
CHEBI:748033 CHEBI
CHEMBL22150 ChEMBL_ID
CHEMBL1889091 ChEMBL_ID
DB08936 DRUGBANK_ID
C084597 MESH_SUPPLEMENTAL_RECORD_UI
2710 PUBCHEM_CID
1301 INN_ID
M26C4IP44P UNII
11602 MMSL
4408 MMSL
d07681 MMSL
003398 NDDF
003399 NDDF
4018770 VANDF
4019672 VANDF
M26C4IP44P INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
biclora HUMAN OTC DRUG LABEL 2 54868-6381 LIQUID 12.50 mg ORAL OTC monograph final 14 sections
AHIST HUMAN OTC DRUG LABEL 1 58407-025 TABLET 25 mg ORAL OTC monograph final 14 sections
STAHIST AD HUMAN OTC DRUG LABEL 2 58407-625 TABLET 25 mg ORAL OTC Monograph Drug 16 sections
BonineKids HUMAN OTC DRUG LABEL 1 63736-044 TABLET, CHEWABLE 25 mg ORAL OTC monograph final 13 sections